Receptor-assisted combinatorial chemistry: thermodynamics and kinetics in drug discovery |
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Authors: | Cheeseman Jeremy D Corbett Andrew D Gleason James L Kazlauskas Romas J |
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Affiliation: | Department of Chemistry, McGill University, 801 Sherbrooke W., Montréal, QC H3A 2K6, Canada. |
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Abstract: | Current drug discovery using combinatorial chemistry involves synthesis followed by screening, but emerging methods involve receptor-assistance to combine these steps. Adding stoichiometric amounts of receptor during library synthesis alters the kinetics or thermodynamics of the synthesis in a way that identifies the best-binding library members. Three main methods have emerged thus far in receptor-assisted combinatorial chemistry: dynamic combinatorial libraries, receptor-accelerated synthesis, and a new method, pseudo-dynamic libraries. Pseudo-dynamic libraries apply both thermodynamics and kinetics to amplify library members to easily observable levels, and attain selectivity heretofore unseen in receptor-assisted systems. |
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Keywords: | combinatorial chemistry drug design inhibitors receptors template synthesis |
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